Nuclei DNA and mitochondria dual damages induced by thiosemicarbazone tripyridyl copper complexes with potential anti-tumor activity

5-Methoxyisatin N(4)-Pyrrolidinyl Thiosemicarbazone (MeOIstPyrd) Restores Mutant p53 and Inhibits the Growth of Skin Cancer Cells, In Vitro

“…In the A431 cell line, the half-life of p53 is 2.5 h, but when treated with MeOIstPyrd, the half-life increases to >8 h. Similarly, in the case of the A549 cell line, the half-life of p53 is approximately 4 h, but in the presence of MeOIstPyrd, the half-life increases to >8 h. This indicates that MeOIstPyrd is increasing the p53 turnover and therefore providing stability. TSCs have been documented to induce DNA break or to possess DNA-binding ability. , DNA being the primary intracellular target for anticancer compounds, we were interested to know if MeOIstPyrd is involved in DNA damage. When an agent interacts with DNA, changes in its absorbance are observed; if a complex intercalates between DNA base pairs, there is generally a small red/blue shift causing a hypochromic effect; conversely, the hyperchromic effect is caused by non-intercalative, electrostatic, or groove binding interactions.…”

“…TSCs have been documented to induce DNA break or to possess DNA-binding ability. 57 , 58 DNA being the primary intracellular target for anticancer compounds, we were interested to know if MeOIstPyrd is involved in DNA damage. When an agent interacts with DNA, changes in its absorbance are observed; if a complex intercalates between DNA base pairs, there is generally a small red/blue shift causing a hypochromic effect; conversely, the hyperchromic effect is caused by non-intercalative, electrostatic, or groove binding interactions.…”

Heteroleptic six-coordinate bismuth(iii) complexes with 2-acetylthiophene thiosemicarbazones: synthesis, characterization, and biological properties

“…[5][6][7] In particular, heterocyclic TSCs attract more attention than aromatic and aliphatic TSCs because they have more donor atoms and therefore can form coordination compounds with more different modes. [8][9][10] Although TSCs show biological activity on their own, it has been shown in many studies that their complexation with a metal increases their biological activity exponentially. [11][12][13] In vitro antitumor activity of 2-acetylthiophene thiosemicarbazone and organoplatin(II) complexes were determined against two different human tumor cell lines (HT-29 and HuTu-80), and it was revealed that these compounds can be considered as agents with potential antitumor activity.…”